Climara Pro

"The U.S. Food and Drug Administration today approved Osphena (ospemifene) to treat women experiencing moderate to severe dyspareunia (pain during sexual intercourse), a symptom of vulvar and vaginal atrophy due to menopause.

The WHI Memory Study (WHIMS)
estrogen plus progestin ancillary study of WHI reported an increased risk of
developing probable dementia in postmenopausal women 65 years of age or older
during 4 years of treatment with daily CE (0.625 mg) combined with MPA (2.5
mg), relative to placebo. It is unknown whether this finding applies to younger
postmenopausal women [see WARNINGS AND PRECAUTIONS, Use in Specific Populations,
and Clinical Studies].

Breast Cancer

In the absence of comparable
data, these risks should be assumed to be similar for other doses of CE and MPA
and other combinations and dosage forms of estrogens and progestins.

Estrogens with or without
progestins should be prescribed at the lowest effective doses and for the
shortest duration consistent with treatment goals and risks for the individual
woman.

Estrogen-Alone Therapy

Endometrial Cancer

There is an increased risk
of endometrial cancer in a woman with a uterus who uses unopposed estrogens.
Adding a progestin to estrogen therapy has been shown to reduce the risk of
endometrial hyperplasia, which may be a precursor to endometrial cancer.

Adequate diagnostic measures, including directed or
random endometrial sampling when indicated, should be undertaken to rule out
malignancy in postmenopausal women with undiagnosed persistent or recurring
abnormal genital bleeding [see WARNINGS AND PRECAUTIONS].

Cardiovascular Disorders and Probable Dementia

Estrogen-alone therapy should not be used for the
prevention of cardiovascular disease or dementia [see WARNINGS AND PRECAUTIONS,
and Clinical Studies].

The WHI estrogen-alone substudy reported increased
risks of stroke and DVT in postmenopausal women (50 to 79 years of age) during
7.1 years of treatment with daily oral CE (0.625 mg)-alone, relative to placebo
[see WARNINGS AND PRECAUTIONS, and Clinical Studies].

The WHIMS estrogen-alone ancillary study of WHI
reported an increased risk of developing probable dementia in postmenopausal
women 65 years of age or older during 5.2 years of treatment with daily CE
(0.625 mg)-alone, relative to placebo. It is unknown whether this finding
applies to younger postmenopausal women [see WARNINGS AND PRECAUTIONS, Use in
Specific Populations, and Clinical Studies].

In the absence of comparable data, these risks should
be assumed to be similar for other doses of CE and other forms of estrogens.

Estrogens with or without progestins should be
prescribed at the lowest effective doses and for the shortest duration
consistent with treatment goals and risks for the individual woman.

DRUG DESCRIPTION

Climara Pro (estradiol/levonorgestrel transdermal system)
is an adhesive-based matrix transdermal patch designed to release both estradiol
and levonorgestrel, a progestational agent, continuously upon application to
intact skin. The 22 cm² Climara Pro system contains 4.4 mg estradiol
and 1.39 mg levonorgestrel and provides a nominal delivery rate (mg per day) of
0.045 estradiol and 0.015 levonorgestrel.

Estradiol USP has a molecular weight of 272.39 and the
molecular formula is C18H24O2.

Levonorgestrel USP has a molecular weight of 312.4 and a
molecular formula of C21H28O2.

The structural formulas for estradiol and levonorgestrel
are:

The Climara Pro transdermal
system comprises 3 layers. Proceeding from the visible surface towards the
surface attached to the skin, these layers are:

A translucent polyethylene backing film.

An acrylate adhesive matrix containing estradiol and
levonorgestrel.

A protective liner of either siliconized or fluoropolymer
coated polyester film. The protective liner is attached to the adhesive surface
and must be removed before the system can be used.

The active components of the
transdermal system are estradiol and levonorgestrel. The remaining components
of the transdermal system (acrylate copolymer adhesive and
polyvinylpyrrolidone/vinyl acetate copolymer) are pharmacologically inactive.

What are the possible side effects of estradiol and levonorgestrel (Climara Pro)?

Stop using this medication and get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have any of the following serious side effects:

What are the precautions when taking estradiol, levonorgestrel transdermal (Climara Pro)?

Before using this medication, tell your doctor or pharmacist if you are allergic to estradiol or levonorgestrel; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.